Cosmetic composition containing uracil-4-carboxylic acid



United States Patent Oflice 3,544,684 Patented Dec. 1, 1970 Int. Cl. A61k 7/00, 27/00 US. Cl. 424-251 2 Claims ABSTRACT OF THE DISCLOSURE Uracil-4-carboxylic acid and its salts increase the softening effect of cosmetic bases.

Cosmetic preparations and devices for the treatment of ageing changes of the skin have the purpose of improving the water absorbing properties of the skin and reducing the formation of wrinkles by stimulating the metabolism. The water absorption as well as the removal of wrinkles can be measured, the latter by determining the depth of the wrinkles.

A suitable method for measuring hydration changes of the skin is e.g. the determination of the resonance frequency. The principle of this measuring method consists in converting electrical oscillations of a frequency generator to mechanical oscillations and applying said mechanical oscillations by means of a pin to the skin. A second pin takes up said oscillations, converts them to electric oscillations, and transmits them to a recorder. The measured resonance frequency measures the ratio of liquid to structured substance. A decrease of tissue fluids, e.g., in atrophied skin, increases the resonance frequency. Juvenile skin with elevated turgor has a lower resonance frequency. When the water absorbency of the skin is improved by suitable cosmetic treatment, the resonance frequency shifts to lower frequencies.

The depth of wrinkles may be measured by combining an impression method with a relief recording method. An impression is made on a suitable material and the impression is measured by means of a relief recorder which converts the unevenness of the impression or mold into electromagnetic oscillations and directly records the same.

It is known that an improved hydration of the skin does not necessarily or inherently smoothen the wrinkles. Numerous compositions which have been investigated influence neither the hydration nor the depth of the wrinkles. Others influence either the hydration or the depth of the wrinkles.

I have now found that uracil-4-carboxylic acid (orotic acid) and its organic and inorganic salts in conventional cream or lotion bases exert a favorable effect on the hydration as well as on the depth of the wrinkles. This is quite surprising because, heretofore, similar effects have been obtained only with placenta extracts and similar mixtures. The described effect was shown only by the uracil-4-carboxylic acid compounds themselves but not by the cosmetic base or additives used.

Suitable cosmetic bases for incorporation of the uracil- 4-carboxylic acid and its salts are conventional water-inoil emulsions, oil-in-water emulsions and/or gelatinous preparations, e.g., of mucilage, or synthetic thickening agents such as polyvinyl pyrrolidone, methyl cellulose, carboxymethyl cellulose. Suitable water-in-oil emulsions are those on the basis of hydrocarbons, fats, lanolin and the like. Oil-in-water emulsions are generally made from saponified fatty acid salts and esters, orthophosphoric acid esters, waxes, lanolin tetraglycol ethers, etc.

The proportion of uracil-4-carboxylic acid in cosmetic bases will be generally about 0.5 to 10 percent by weight.

The effect of the composition according to the invention on the hydration of the skin and the depth of the wrinkles depends on the frequency of application and is always observable after several days use. The effect is present still 24 hours after the last application; this shows that the composition penetrates into, and influences, also the deeper layers of the skin.

When determined as described hereinabove, the novel cosmetic composition produces a long-term reduction of the wrinkle depth which is about 50% of the short-term reduction produced by preparations that have a purely physical tightening effect. Such preparations, e.g., those on the basis of chicken egg white, serum albumin and globulin, reduce, after drying of the applied solution, the depth of wrinkles by about 30 percent. However, this effect remains only a short time and is removed by washing.

Uracil-4-carboxylic acid is found in milk as precursor of the pyrimidines and nuclei acid. It has particularly a growth stimulating effect, which is utilized therapeutically in oral and parenteral pharmaceutical compositions. Also in larger dosages, the compound is readily tolerated, and the skin is not affected even by prolonged and regular use.

The uracil-4-carboxylic acid is diflicultly soluble in water. Higher concentrations can be obtained by addition of a coupling agent, e.g., methyl glucamine.

Some cosmetic preparations according to the invention are given in the following examples. All parts are given by weight.

EXAMPLE 1 Water-containing lanolin alcohol ointment 90.0 Uracil-4-carboxylic acid 5.0 Liquid parafiin 5.0

EXAMPLE 2 Cety stearyl alcohol 6.0 Ointment bases of tert. ester of orthophosphoric acid and lanolin alcohol tetraglycol ether 10.0

Glycerol 5.0 Choline salt of uracil-4-carboxylic acid 6.0 Water ad 100.0.

EXAMPLE 3 Tragacanth 5.0 Glycerol 5.0 Uracil-4-carboxylic acid 3.0 Methyl glucamine 4.0 p-Oxybenzoic acid ester (preservative) 0.2 Water ad 100.0.

EXAMPLE 4 Stearic acid 18.0 Almond oil 2.0 Cetyl alcohol 0.6 Triethanolamine 3.0 Glycerol I 8.0 Uracil-4-carboxylic acid 3.0 p-Oxybenzoic acid ester (preservative) 0.2 Water ad 100.0.

EXAMPLE 5 Beeswax (bleached) 10.0 Peanut oil 30.0 Spermaceti 3.0 Lanolin 3.0 Glycerol 5.0 Uracil-4-carboxylic acid 4.0 Methylglucamine 5.0 p-Oxybenzoic acid ester (preservative) 0.2 Water ad 100.0.

r If .compositionsncontaining uracilr-4-carboxylic acid or its salts are to be used for face masks, e.g., foam masks, they are used preferably as aerosols with addition of a foam stabilizer such as a salt 'of a condensation product of a saturatedfatty acid of medium chain length and sarcosine.

I claim: a

1. A cosmetic preparation for increasing hydration of the skin and producing along-lasting reduction of wrinkle depth consisting essentially of an aqueous cosmetic cream or lotionbase having incorporated therein about 0.5 to 10 percent .-by weight of a member of the the solubility of the uracil-4-carboxylic -acid component in said aqueous cosmetic base.

group consistingof uracil-4-carboxylic acid and the choline salt of said acid.

2. The cosmetic preparation of claiml containing 15 also methyl glucamine in an amount sufiicient to increase References Cited UNITED STATES PATENTS 2/1944- Stambovsky 424310X 1/1964 Ferguson, Jr.-- 424351X OTHER REFERENCES I Us. c1; JR. 

